AKT as a therapeutic target for cancer

M Song, AM Bode, Z Dong, MH Lee - Cancer research, 2019 - AACR
Many cellular processes in cancer are attributed to kinase signaling networks. V-akt murine
thymoma viral oncogene homolog (AKT) plays a major role in the PI3K/AKT signaling …

AKT/PKB signaling: navigating the network

BD Manning, A Toker - Cell, 2017 - cell.com
The Ser and Thr kinase AKT, also known as protein kinase B (PKB), was discovered 25
years ago and has been the focus of tens of thousands of studies in diverse fields of biology …

New perspectives for targeting RAF kinase in human cancer

Z Karoulia, E Gavathiotis, PI Poulikakos - Nature Reviews Cancer, 2017 - nature.com
The discovery that a subset of human tumours is dependent on mutationally deregulated
BRAF kinase intensified the development of RAF inhibitors to be used as potential …

PI3K and cancer: lessons, challenges and opportunities

DA Fruman, C Rommel - Nature reviews Drug discovery, 2014 - nature.com
The central role of phosphoinositide 3-kinase (PI3K) activation in tumour cell biology has
prompted a sizeable effort to target PI3K and/or downstream kinases such as AKT and …

The translational landscape of mTOR signalling steers cancer initiation and metastasis

AC Hsieh, Y Liu, MP Edlind, NT Ingolia, MR Janes… - Nature, 2012 - nature.com
The mammalian target of rapamycin (mTOR) kinase is a master regulator of protein
synthesis that couples nutrient sensing to cell growth and cancer. However, the downstream …

Ten things you should know about protein kinases: IUPHAR R eview 14

D Fabbro, SW Cowan‐Jacob… - British journal of …, 2015 - Wiley Online Library
Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

PI Poulikakos, C Zhang, G Bollag, KM Shokat, N Rosen - Nature, 2010 - nature.com
Tumours with mutant BRAF are dependent on the RAF–MEK–ERK signalling pathway for
their growth,,. We found that ATP-competitive RAF inhibitors inhibit ERK signalling in cells …

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

G Hatzivassiliou, K Song, I Yen, BJ Brandhuber… - Nature, 2010 - nature.com
Activating mutations in KRAS and BRAF are found in more than 30% of all human tumours
and 40% of melanoma, respectively, thus targeting this pathway could have broad …

[HTML][HTML] Discovery of small molecule cancer drugs: successes, challenges and opportunities

S Hoelder, PA Clarke, P Workman - Molecular oncology, 2012 - Elsevier
The discovery and development of small molecule cancer drugs has been revolutionised
over the last decade. Most notably, we have moved from a one-size-fits-all approach that …

The nuts and bolts of AGC protein kinases

LR Pearce, D Komander, DR Alessi - Nature reviews Molecular cell …, 2010 - nature.com
The AGC kinase subfamily of protein kinases contains 60 members, including PKA, PKG
and PKC. The family comprises some intensely examined protein kinases (such as Akt, S6K …